Fructus Extract Research Articles

Effects of health functional foods on Cytochrome P450 enzymes

Increasing evidence has shown the involvement of health functional foods (HFFs) in inhibition or induction of cytochrome P450 (CYP), affecting the pharmacokinetics of co-administered drugs. To optimize the use of HFFs, it is nec-essary to understand the effects of them on CYPs. In this review we summarize the findings from clinical and in vitro studies evaluating the effects of HFFs on CYPs. In in vitro studies, CYP2C9 and 3A4 were strongly inhibited by allicin in garlic, boswellia extract, fermented curcuma, licorice extract, pomegranate concentrate, and red yeast rice. Furthermore, CYP2C9 was suppressed by hydrolyzed soy extract, lycii fructus extract, and Rhus verniciflua extract. Moreover, red yeast rice strongly inhibited CYP2D6, whereas CYP 2C19 was strongly suppressed by garlic, licorice extract, lycii fructus extract, red yeast rice, and Rhus verniciflua extract. Meanwhile, ginkgo biloba leaf extract showed a potent inductive effect on CYP2C19. In clinical studies, the long-term consumption of ginseng or ginkgo biloba leaf extract caused moderate inductive effects on CYP3A, whereas intake of milk thistle extract led to a moderate inhibition of CYP2C9. Further clinical studies are needed to verify the effects of HFFs on CYPs.

음경해면체 이완작용에 미치는 蛇床子의 효과

In order to define the effect of Torilis Fructus(TF) extract which has been used for the treatment of erectile dysfunction, experiments were carried out by organ bath study, histochemical and immunohistochemical methods. First, in the organ bath study, when TF extract was administered to the maxillary contracted corpus cavernosum by PE (10-6 M), there was a significant relaxation effect on corpus cavernosum at concentration of 1, 3 ㎎/㎖. Compared with the absence of L-NNA pretreatmen, pretreatment of L-NNA was inhibited the relaxation effect of penile corpus cavernosum. In the immunohistochemical study, the eNOS positive reaction was significantly increased, and the PDE5 positive reaction was significantly decreased due to the administration of TF extract. Therefore, it show that the TF enhances the production of eNOS and NO, inhibits PDE5 which blocks the action of increased cGMP, relaxes the corpus cavernosum. So TF relaxes the corpus cavernosum and it can be used as a safer erectile dysfunction treatment.

Protective effects of Alpinae Oxyphyllae Fructus extracts on lipopolysaccharide-induced animal model of Alzheimer's disease

Ethnopharmacological relevanceAlpinae Oxyphyllae Fructus (AOF) with warming and tonifying the kidney and spleen, anti-salivation, anti-polyuria and anti-diarrhea functions is the dried ripe fruits of Alpinia oxyphylla Miq. (Zingiberaceae). As a traditional Chinese medicine, its application history is very long. Aims of the studyThe purpose of our study is to investigate the effects of different solvent extracts from AOF on lipopolysaccharide (LPS)-induced animal model of Alzheimer's disease (AD) to elucidate the traditional medical theories with modern pharmacological methods and provide a reference for further clarifying its active components and mechanisms. Materials and methodsThe method of stepwise screening was adopted in this paper. The animals were divided into 9 groups, including control (CT) group, model (MD) group, donepezil (DPZ) group, total extract (TT) group, petroleum ether extract (PE) group, chloroform extract (CF) group, ethyl acetate extract (EA) group, n-butanol extract (NB) group and water extract (WT) group. The anti-amnesic effects of different solvent extracts from AOF were measured in LPS-induced memory deficits mice by Y maze test and Morris water maze (MWM) test. Hematoxylin eosin (HE) staining was applied to observe pathological changes in hippocampus and cerebral cortex tissue of different groups. Biochemical indicators including ionized calcium-binding adaptor molecule 1 (IBA-1), interleukin beta 1 (IL-1β), Aβ1–42 and hyperphosphorylated tau proteins (p-tau) in hippocampus and cortex after treatment with LPS were measured according to the manufacturer's instructions of ELISA kits. HPLC was used to evaluate the major components of different extracts. ResultsIt was found that successive intragastric administration of AOF (360 mg/kg) extracts for 14 days showed different degrees of improvement on LPS-induced AD model as measured by Y-maze test, Morris water maze test, and Histopathological examination. Moreover, the results of ELISA suggested petroleum ether (PE) extracts were worth recommending for inhibiting the high level of IBA-1, IL-1β, Aβ1–42 and p-tau in hippocampus and cortex after treatment with LPS. ConclusionsThe present study demonstrated for the first time that AOF attenuated LPS-induced learning and memory impairment, which may be associated with its inhibitory effect on neuroinflammation, amyloids-β (Aβ) deposition and p-tau. This research provided a theoretical basis for elucidating the traditional theory of AOF, and was also the stepping stone to the next step.

Comparative pharmacokinetics of triterpenic acids in normal and immunosuppressed rats after oral administration of Jujubae Fructus extract by UPLC-MS/MS

The fruit of Ziziphus jujuba (Jujubae Fructus) has been used as food and crude drug for thousands of years. Although several chemical and biological studies have revealed triterpenic acid as the main bioactive constituent of Jujubae Fructus responsible for immune-regulatory activity, only few pharmacokinetic studies have been conducted. To comprehend the kinetics of triterpenic acids and promote their curative application, a sensitive and efficient ultra-performance liquid chromatography coupled with mass spectrometry method (UPLC-MS/MS) was established. UPLC-MS/MS was applied for the simultaneous determination of ceanothic acid, epiceanothic acid, pomonic acid, alphitolic acid, maslinic acid, betulinic acid, and betulonic acid in normal and immunosuppressed rat plasma samples. After sample preparation, chromatographic separation was performed on an Acquity UPLC BEH C18 column (2.1 × 100 mm, 1.7 μm) with acetonitrile: methanol (1:1, v/v) and 0.5% ammonium acetate in water as mobile phase. The established method was validated and found to be specific, accurate, and precise for the seven triterpenic acids, and was successfully applied for the pharmacokinetic study of rat plasma samples. The results showed that the pharmacokinetic parameters (Cmax, Tmax, AUC0–t, AUC0–∞, and CLz/F) in the plasma samples of immunosuppressed rats were significantly different from those in normal rats, and might provide an insight for the clinical usage of triterpenic acids from Jujubae Fructus.

European Ethnopharmaceuticals for Self-Medication in Japan: Review Experience of Vitis vinifera L., Folium Extract and Vitex agnus-castus L., Fructus Extract as OTC Drugs.

Since the publication of “Application Guideline for Western Traditional Herbal Medicines as OTC Drugs” in 2007, only two European ethnopharmaceuticals, Vitis vinifera L., folium extract (Antistax) and Vitex agnus-castus L., fructus extract (Prefemin), have been approved as OTC drugs in Japan. In this review, we describe the current regulation of Western ethnopharmaceuticals in Japan, summarize our regulatory experiences and discuss the scientific and regulatory issues involved.

Anti-allergic and anti-atopic dermatitis effects of Gardenia Fructus extract

ABSTRACT Atopic dermatitis (AD) is a common allergic, inflammatory skin disease. Here, we focused on the anti-allergic and anti-inflammatory effects of Gardenia jasminoides Ellis fructus extracts (GFE) in DNCB treated NC/Nga mice. In an in vivo study, GFE treatment significantly decreased immunoglobulin E (IgE) levels and cytokines expression in spleen and serum of treatment groups mice, compared with the negative controls (administered 0.2% DNCB only). Mice treated with GFE had fewer inflammatory cell infiltrates in the dermis and hypodermis compared to the negative controls. In addition, we also studied β-Hexosaminidase release assay and possible anti-inflammatory mechanism of GFE in RBL-2H3 cells. GFE suppressed the expression of COX-2 and TNF-α, the translocation of NF-κβ, and the phosphorylation of Syk, p38, JNK, and Erk1/2 in stimulated RBL-2H3 cells. These results strongly suggest that GFE inhibits the allergic response by reducing mast cell activation and may have therapeutic potential as an anti-atopic dermatitis agent.

Muscle-protective effects of Schisandrae Fructus extracts in old mice after chronic forced exercise

Ethnopharmacological relevanceSchisandrae Fructus (SF), the dried fruit of Schisandra chinensis (Turcz.) Baill., is a well-known traditional herb used in Asia for enhancing physical work capacity as well as providing anti-stress and anti-inflammatory effects. Extracts of SF (SFe) have also been reported to increase skeletal muscle mass and inhibit muscle atrophy. Aim of the studyWe examined whether SFe had muscle-protective effects in old mice after chronic forced exercises, and, if so, relevant mechanisms. Materials and methodsTen-month-old aged male mice were divided into six groups. One group received no forced swimming after oral administration of distilled water (Intact); the other groups received forced swimming after administration of distilled water (SW), oxymetholone (OXY), or SFe at 500, 250 and 125mg/kg (SFe500, SFe250, and SFe125, respectively). Forced swimming was conducted for 2min at 30min after oral administration; the treatment was repeated for 28 days. Muscle thickness, weight, lean proportion, and strength were examined. The sampled muscles were subjected to histopathological and biochemical analyses. Plasma was examined by biochemical analyses. ResultsThe thicknesses of the calf muscle and the sampled gastrocnemius and soleus, protein proportion and muscle strength increased significantly in the SW group versus Intact, and they were further increased in the SFe and OXY groups versus SW. The forced swimming in the SW group upregulated mRNA expression related to protein synthesis (Akt1, PI3K) and muscle growth (A1R, TRPV4), while it downregulated mRNAs related to protein degradation (atrogin-1, MuRF1) and muscle growth inhibitor (myostatin, SIRT1). The detected upregulation and downregulation were enhanced in the SFe groups. In addition, the SFe administration inhibited lipid peroxidation and reactive oxygen species, and accelerated activities of endogenous anti-oxidants and anti-oxidant enzymes. Plasma biochemistry showed decreases in creatine, creatine kinase and LDH in the SFe groups versus SW, suggesting muscle-protective effects of SFe. In the SFe groups versus SW, histopathological analyses revealed an increase in myofibre diameter, and immunohistochemistry showed increases in myofibres immunoreactive for ATPase and decreases in myofibres for apoptosis markers (caspase-3, PARP) and oxidative stress markers (NT, 4HNE, iNOS). ConclusionsOral administration of SFe, especially SFe500, enhanced exercise-induced adaptive muscle strengthening in aged mice after forced swimming through anti-apoptotic and anti-oxidant effects, mediated via modulation of gene expression related to muscle synthesis or degradation. These results suggest that SFe may be helpful in improvement various muscle disorders as an adjuvant therapy to exercise-based remedies.

Inhibition of Mast Cell-Mediated Allergic Responses by Arctii Fructus Extracts and Its Main Compound Arctigenin.

The Arctium lappaseeds (Arctii Fructus) and its major active compound, arctigenin (ARC), are known to have anticancer, antiobesity, antiosteoporosis, and anti-inflammatory activities. However, the effect of Arctii Fructus and ARC on mast cell-mediated allergic inflammation and its associated mechanism have not been elucidated. Therefore, we attempted to investigate the antiallergic activity of Arctii Fructus and ARC on mast cells and experimental mouse models. Arctii Fructus water extract (AFW) or ethanol extract (AFE) and ARC reduced the production of histamine and pro-inflammatory cytokines such as interleukin (IL)-1β, IL-6, IL-8, and TNF-α in mast cells. AFW, AFE, and ARC inhibited phosphorylation of MAPKs and NF-κB in activated mast cells. Moreover, IgE-mediated passive cutaneous anaphylaxis and compound 48/80-induced anaphylactic shock were suppressed by AFW, AFE, and ARC administration. These results suggest that Arctii Fructus and ARC are potential therapeutic agents against allergic inflammatory diseases.

A sensitive UHPLC-MS/MS method for the simultaneous quantification of three lignans in human plasma and its application to a pharmacokinetic study.

The aim of this study was to develop an analytical method to simultaneously analyze schizandrin, schizandrol B, and gomisin N lignans in human plasma using ultra high performance liquid chromatography with tandem mass spectrometry. The three lignans were separated using a mobile phase of water and acetonitrile containing 0.02% acetic acid equipped with a Kinetex C18 column (2.1mm×50mm, 1.7μm). This analysis was achieved by multiple reaction monitoring mode in an electrospray interface. The mass transitions were m/z 433.1→384.0 for schizandrin, 398.8→367.8 for schizandrol B, and 400.6→299.8 for gomisin N. Liquid-liquid extraction with methyl tert-butyl ether was used to obtain the three lignans. The chromatograms showed high resolution, sensitivity, and selectivity with no interference with plasma constituents. The calibration curves for the three lignans in human plasma were 0.05-50ng/mL and displayed excellent linearity with correlation coefficients greater than 0.99. Precision for all three lignans was within 11.23%. The accuracy was 88.3-99.0% for schizandrin, 90.6-103.4% for schizandrol B, and 90.2-103.5% for gomisin N. The developed simultaneous analytical method satisfied the criteria of international guidance and could be successfully applied to the pharmacokinetic study of three lignans after oral administration of Schisandrae Fructus extract powder to humans.

Inhibitory effects of Ponciri Fructus on testosterone-induced benign prostatic hyperplasia in rats

BackgroundBenign prostatic hyperplasia (BPH) is non-cancerous condition of enlargement of the prostate, a common occurrence in older men. The immature fruits of Poncirus trifoliata (L.) Rafinesque (Rutaceae), Ponciri Fructus are widely used in traditional oriental medicine for the therapy of various diseases. However, little is known about the mechanism underlying the pathogenesis of BPH. In the present study, we investigated the protective effects of a Ponciri Fructus extract (PFE) on the development of BPH in a in a rat model of BPH induced by testosterone propionate (TP).MethodsMale Sprague Dawley rats were used as a model of BPH after its induction by daily subcutaneous injections of TP/corn oil, for a period of four weeks. PFE was administrated daily 1 h before TP/corn oil injection by oral gavage at a dose level of 200 mg/kg during the 4 weeks of TP/corn oil injections. All rats were sacrificed at the end of the experiment, we measured the relative prostate weight, the levels of testosterone and dihydrotestosterone (DHT), histological changes, activities of antioxidant enzymes (catalase, glutathione peroxidase, glutathione reductase, and superoxide dismutase), and expression of proliferating cell nuclear antigen (PCNA). In addition, we also measured the inhibition (%) of 5α-reductase in the prostatic tissue.ResultsOur findings indicate that PFE significantly inhibited the development of BPH; decreased the relative prostate weight, the level of testosterone and DHT in serum and prostatic tissue, prostatic hyperplasia, expression of PCNA, and increased the antioxidant enzymes. Moreover, PFE showed a weak inhibitory activity on 5α-reductase.ConclusionsThese results suggest that PFE may be used as a therapeutic agent for BPH via antiproliferative and antioxidant effects.

회화나무(Sophora japonica L.) 꽃(괴화)과 열매(괴각)의 미백활성 평가

회화나무는 한의학에서 간과 혈관계 질환의 치료에 사용되어온 약용 식물로, 그 꽃과 열매를 괴화와 괴각이라 한다. 괴화와 괴각은 메탄올 추출물로부터 에틸아세테이트 분획물을 얻어 시료로 사용하였고, B16 F10 세포를 이용하여 Western blot을 실행하였다. 미백효과를 확인하기 위해, tyrosinase, TRP-1, TRP-2, MITF 단백질을 확인하였다. 그 결과, 괴화와 괴각 추출물은 세포 생존율에는 영향이 미미하였으며, 모두tyrosinase, TRP-1, TRP-2, MITF 단백질의 발현 억제효과를 나타냈다. 또한 농도 의존적으로 억제효과를 보였으며, 이를 통해 전통적으로 사용되어 왔던 괴화와 괴각은 기능성 화장품의 원료와 같은 천연식물 유래 자원으로 상당한 가치를 나타냈다. Sophora japonica has been used for treatment of liver and blood-related diseases in herbology. We evaluated whitening activities of Sophorae Flos and Fructus. Sophorae Flos and Fructus were extracted with methanol (MeOH) and divided into petroleum ether, ethyl acetate(EtOAC) and water fraction. For whitening effect by western blot in B16 F10 cells, we analyzed it by investigating the effect of tyrosinase, TRP-l (tyrosinase-related protein 1), TRP-2 (tyrosinase-related protein 2) and MITF (microphthalmia-associated transcription factor) protein expression. The protein expressions of tyrosinase, TRP-1, TRP-2 and MITF in B16 F10 cells treated with Sophorae Flos and Fructus extract were reduced in a dose-dependant manner. Therefore, these results suggest that Sophorae Flos and Fructus have useful plant resource to be developed as functional cosmetic.

An integrated strategy using UPLC–QTOF-MSE and UPLC–QTOF-MRM (enhanced target) for pharmacokinetics study of wine processed Schisandra Chinensis fructus in rats

Currently the pharmacokinetic (PK) research of herbal medicines is still limited and facing critical technical challenges on quantitative analysis of multi-components from biological matrices which often accompanied by lacking of authentic standards and low concentration. This present work contributes to the development of an integrated strategy for extensive pharmacokinetics assessments, and a selective and sensitive method independent of authentic standards for multi-components analysis based on the use of ultra-performance liquid chromatography/quadrupole-time-of-flight/MSE (UPLC-TOF-MSE) and UPLC-TOF-MRM (rnhanced target). Initially, phytochemicals were identified by UPLC-TOF-MSE analysis, subsequently the identified components were matched with authentic standards and pre-classified, and UPLC–QTOF-MRM method optimized and developed. To guarantee reliable results, three rules are necessary: (1) detection with a mass error of less than 5ppm; (2) same class chemical compositions with structural high similarity between analytes with and without authentic reference substance; (3) a matching retention time between TOF-MRM mode and TOF-MSE within 0.2min. The developed and validated method was applied for the simultaneous determination of 12 lignans in rat plasma after administered with wine processed Schisandra Chinensis fructus (WPSCF) extract. Such an approach was found capable of providing extensive pharmacokinetic profiles of multi-components absorbed into blood after oral administrated with WPSCF extract. The results also indicated that significant difference in pharmacokinetics parameters of dibenzocyclooctadiene lignans was observed between schizandrin and gomisin compounds. For lignans, the absorption via gastrointestinal tract were all rapid and maintained relatively long retention time, especially for schisantherin A and schisantherin B with higher plasma exposure.

Comparative studies on the multi-component pharmacokinetics of Aristolochiae Fructus and honey-fried Aristolochiae Fructus extracts after oral administration in rats

BackgroundAristolochiae Fructus (AF) and honey-fried Aristolochiae Fructus (HAF) have been used in China for a long time as anti-tussive and expectorant drugs. Few clinical cases have been reported to be associated with the toxicity of AF and HAF, although relatively high amounts of aristolochic acids (AAs) have been found in them. Our previous experiments have verified from the chemical changes and from traditional toxicology that honey-processing can significantly reduce the toxicity of AF. To further elucidate the detoxification mechanism of honey-processing, comparative pharmacokinetics of AAs in AF and HAF are performed in this study.MethodsAn HPLC-MS/MS (high-performance liquid chromatography-tandem mass spectrometry) method was developed and validated for the determination of AA I, AA II, AA C, AA D and 7-OH AA I in rat plasma. The multi-component pharmacokinetics of AAs in AF and HAF extracts were investigated after the oral administration of three doses to rats. The relative pharmacokinetic parameters were compared systematically.ResultsThe five AAs shared a similar nonlinear PK (pharmacokinetic) process. They involve rapid absorption and elimination, and they were fit into a two-compartmental open model. Some significant pharmacokinetic differences were observed between the AF and HAF groups: the Cmax and AUC values of AA I and AA II in the AF groups were much higher than those of the HAF groups.ConclusionsHoney-frying technology can reduce the toxicity of AF by significantly decreasing the absorption of AA I and AA II. The PK parameters obtained in this work could provide valuable references for the toxicity research and clinical use of Aristolochiaceae herbs, including AF and HAF.Graphical abstractProcess diagram of comparative pharmacokinetics study

산수유(Corni fructus) 분획 추출물의 항산화 활성 및 RAW 264.7 대식세포에서 염증매개물질 억제 효과

The antioxidant and anti-inflammatory effects of Corni fructus extracts (CEF, EtOAc extraction; CBF, buthanol extraction; CWF, water extraction) were investigated. The total phenolics of CEF (173.3 mg TAE/g) were significantly higher than those of CWF (26.7 mg TAE/g) and CBF (94.8 mg TAE/g). DPPH and ABTS free radical scavenging activity of CEF (DPPH: RH50; 25.1 μg/mL, ABTS: RC50; 36.1 μg/mL) showed even higher than that of BHA and α-tocopherol used as positive control. All three Corni fructus extracts in the concentration of 1~100 μg/mL were effective inhibitors of NO and prostaglandin E2 (PGE2). NO production was inhibited 71.3~92.2% by CEF, 76.8~85.5% by CBF and 74.4~96.9% by CWF, respectively. CEF, CBF and CWF (1~100 μg/mL) inhibited also pro-inflammatory cytokines like TNF-α, IL-1β and IL-6 very effectively. TNF-α was inhibited up to 51.2% by CWF and IL-1β was inhibited up to 67.1% by CEF. IL-6 was best inhibited by CEF up to 58.9%. This study suggested the potential of Corni fructus for use as an excellent antioxidant substance and inflammatory inhibiting mediators. Therefore CEF, CBF and CWF Corni fructus extracts may be used for therapeutic approach to various inflammatory diseases.

Akt activation by Evodiae Fructus extract protects ovary against 4-vinylcyclohexene diepoxide-induced ovotoxicity

Ethnopharmacological relevanceEvodiae Fructus (EF) is the dried, unripe fruit of Evodia rutaecarpa Benth., and one of the main components of traditional herbal prescriptions issued for the treatment of sterility caused by irregular menstruation in Korea. However, scientific evidence regarding the efficacy and action mechanism of EF is lacking. Aim of the studyIn this study, the authors established an in vitro screening tool to identify promising new drug candidates in herbal medicines for the prevention and treatment of premature ovarian failure. The protective effects of EF extracts against 4-vinylcyclohexene diepoxide (VCD)-induced ovotoxicity were investigated and the molecular mechanism responsible was sought. Material and MethodsEF extract was prepared by boiling EF in water and its quality was confirmed by high performance liquid chromatography. CHO-K1 (Chinese hamster ovary cells) and COV434 (human ovarian granulosa cells) cells were plated, pretreated with EF extract for 2h and then treated with 1.5mM or 0.5mM VCD for 24h, respectively. Cell viabilities were measured using an MTT assay, and protein levels were determined by western blotting. ResultsVCD significantly suppressed the viability of both CHO-K1 and COV434 cells in a dose-dependent manner and induced the apoptosis of CHO-K1 cells at 1.5mM. EF extract dose-dependently blocked the ovotoxicity induced by treatment with VCD. Furthermore, EF extract significantly activated Akt and downstream effectors such as mTOR and GSK-3β in CHO-K1 cells. The ability of EF extract to prevent cytotoxicity by VCD was antagonized by pretreatment of LY294002, a PI3K/Akt inhibitor. ConclusionEF has the ability to protect ovary cells against VCD-induced ovotoxicity, probably via Akt activation. These results suggest that the beneficial effects of EF might be useful for preventing premature ovarian failure or unexplained infertility caused by environmental factors.

Protective effect of Evodiae Fructus extract against 4-vinylcyclohexene diepoxide- induced ovotoxicity in CHO-K1 cells

Protective effect of Evodiae Fructus extract against 4-vinylcyclohexene diepoxide- induced ovotoxicity in CHO-K1 cells

Antioxidant Effects and Storage Stability of Yanggaeng Supplemented with Lycii Fructus Extract

The purpose of this study was to investigate the antioxidant effects and storage stability of Yanggaeng prepared with Lycii fructus extract (LY). Lycii fructus extract was added at 0 (C), 1.5 (LY1), 3.0 (LY2), 4.5 (LY3), and 6% (LY4) (w/w), and then total phenol contents, DPPH radical inhibition, ABTS radical inhibition, and physiology of microorganisms were measured. The total phenol content of LY1-LY4 was higher than that of control Yanggaeng. LY4 showed the strongest DPPH radical inhibition of 52.51%, whereas the DPPH radical inhibition of the control was the lowest. Additionally, ABTS radical inhibition increased in accordance with an increase in the concentration of Lycii fructus extract. Microbiological analysis revealed that LY1-LY4 showed lower variation in total cell count, mold, and yeast content compared to control Yanggaeng during the storage period.

Anti-aging Effect of Psoraleae Fructus Extract in UVA-irradiated HaCaT Cells

목적: 본 연구는 보골지 열수 추출물의 자외선에 의해 노화가 유도된 HaCaT 세포의 항노화 효과를 확인하기 위하여 수행되었다. 방법: 자외선에 의해 노화가 유도된 HaCaT 세포에서 보골지 열수 추출물의 항노화 효능을 확인하 기 위해서 보골지 열수 추출물의 농도별 세포 생존률, mRNA의 발현 양상, 히알루론산 단백질의 생성 정도를 확인하였다. 결과: 보골지 열수 추출물의 항노화 효과를 확인하기 위하여A QP3, HAS2, KRT1, KRT10의 유전자 발현을 확인한 결과, 자외선에 의해 감소한 AQP3와 HAS2 유전자의 발현이 보골지 열수 추출물에 의해 각각 2.5배, 2.8배 증가하였 다. 각질형성세포의 과각질화에 관여하는 KRT1 과 KRT10 의 유전자 발현은 보골지 열수 추출물에 의해 각각 30%, 50% 감소함을 확 인하였다. 또한 히알루론산 단 백질의 생성이 보골지 열수 추출물에 의해 38% 가량 증가됨을 확인하였다. 따라서 본 연구자는 보 골지 열수 추출물의 보습효과 및 항노화 효능을 확인하였다. 결론: 본 연구결과를 통하여 보골지 열수 추출물의 항노화 효능을 확인하였고, 향후 보골지 열수 추 출물이 화장품 및 건강식품과 의약품의 개발에 응용될 수 있는 소재로서의 가능성을 확인하기 위해 추가적인 기전연구가 필요할 것으로 생각된다.

Hepatoprotective effects of hoveniae semen cum fructus extracts in ethanol intoxicated mice.

[Purpose]The objective of this study was to evaluate the hepatoprotective effects of Hoveniae Semen Cum Fructus extract in ethanol induced hepatic damages.[Methods]Hepatic damages were induced by oral administration of ethanol and then Hoveniae Semen Cum Fructus extract was administered.[Results]Following Hoveniae Semen Cum Fructus extract administration, body and liver weights were increased, while aspartate aminotransferase, alanine aminotransferase, albumin, γ-glutamyl transferase, and triglyceride levels in the serum, triglyceride contents, tumor necrosis factor -α level, cytochrome (CY) P450 2E1 activity in the liver and mRNA expression of hepatic lipogenic genes, and Nitrotyrosine and 4-HNE-immunolabelled hepatocytes were decreased. However, mRNA expression of genes involved in fatty acid oxidation was increased. Also, as a protective mechanism for hepatic antioxidant defense systems, decreased liver MDA contents, increased glutathione contents, increased dismutase and catalase activities were observed when compared to the ethanol control.[Conclusion]Hoveniae Semen Cum Fructus extract favorably protected against liver damages, mediated by its potent anti-inflammatory and anti-steatosis properties through the augmentation of the hepatic antioxidant defense system by NF-E2-related factor-2 activation, and down-regulation of the mRNA expression of hepatic lipogenic genes or up-regulation of the mRNA expression of genes involved in fatty acid oxidation.

In vitro protective effects of Hoveniae Semen cum Fructus extracts against oxidative stress

We evaluated the in vitro cytoprotective effects of Hoveniae Semen cum Fructus (HSCF) extracts against oxidative stress-mediated cell damage using HepG2 cells. Cytotoxic effects of HSCF extracts were observed in HepG2 cells, and the 50% inhibitory concentration was determined. Cytoprotective effects of sublethal doses of HSCF extracts were evaluated using a tert-butyl hydroperoxide (tBHP)-induced cellular damage model. We also assessed whether NFE2-related factor-2 (Nrf2) was transactivated by HSCF extracts. The antioxidant capacity of HSCF extracts was evaluated with superoxide dismutase (SOD) and catalase (CAT) activities and the expression of the antioxidant genes glutamate cysteine ligase catalytic subunit (GCLC), hemeoxygenase-1 (HO1), and NAD (P)H dehydrogenase quinone 1 (NQO1). HSCF extracts up to 1,000 μg/mL showed no cytotoxic effect in HepG2 cells. Indeed, 300 and 1,000 μg/mL of HSCF extracts significantly protected HepG2 cells from oxidative stress-mediated cell death by tBHP. As a molecular mechanism, HSCF extracts at 1,000 μg/mL significantly increased Nrf2 transactivation and induced expression of its target genes (GCLC, HO1, NQO1). Furthermore, 1,000 μg/mL of HSCF extracts enhanced SOD activity. Although treatment with 300 and 1,000 μg/mL of HSCF extracts tended to slightly increase CAT activity, the increases were not statistically significant. These findings provide direct evident that HSCF extracts have favorable hepatoprotective effects against oxidative stress through Nrf2-mediated antioxidant gene induction.